Boucher Guillaume, Said Bilal, Ostler Elizabeth L, Resmini Marina, Brocklehurst Keith, Gallacher Gerard
School of Pharmacy and Biomolecular Sciences, University of Brighton, Cockcroft Building, Lewes Road, Moulsecoomb, Brighton BN2 4GJ, UK.
Biochem J. 2007 Feb 1;401(3):721-6. doi: 10.1042/BJ20060551.
A kinetically homogeneous anti-phosphate catalytic antibody preparation was shown to catalyse the hydrolysis of a series of O-aryl N-methyl carbamates containing various substituents in the 4-position of the O-phenyl group. The specific nature of the antibody catalysis was demonstrated by the adherence of these reactions to the Michaelis-Menten equation, the complete inhibition by a hapten analogue, and the failure of the antibody to catalyse the hydrolysis of the 2-nitrophenyl analogue of the 4-nitrophenylcarbamate substrate. Hammett sigma-rho analysis suggests that both the non-catalysed and antibody-catalysed reactions proceed by mechanisms in which development of the aryloxyanion of the leaving group is well advanced in the transition state of the rate-determining step. This is probably the ElcB (elimination-addition) mechanism for the non-catalysed reaction, but for the antibody-catalysed reaction might be either ElcB or B(Ac)2 (addition-elimination), in which the elimination of the aryloxy group from the tetrahedral intermediate has become rate-determining. This result provides evidence of the dominance of recognition of phenolate ion character in the phosphate hapten in the elicitation process, and is discussed in connection with data from the literature that suggest a B(Ac)2 mechanism, with rate-determining formation of the tetrahedral intermediate for the hydrolysis of carbamate substrates catalysed by an antibody elicited by a phosphonamidate hapten in which phenolate anion character is minimized. The present paper contributes to the growing awareness that small differences in the structure of haptens can produce large differences in catalytic characteristics.
一种动力学均相的抗磷酸催化抗体制剂被证明能催化一系列在O-苯基的4-位含有各种取代基的O-芳基N-甲基氨基甲酸酯的水解反应。这些反应符合米氏方程、被半抗原类似物完全抑制以及该抗体不能催化4-硝基苯基氨基甲酸酯底物的2-硝基苯基类似物的水解反应,从而证明了抗体催化的特异性。哈米特σ-ρ分析表明,非催化反应和抗体催化反应均通过离去基团的芳氧基阴离子在速率决定步骤的过渡态中充分发展的机制进行。这可能是非催化反应的ElcB(消除-加成)机制,但对于抗体催化反应可能是ElcB或B(Ac)2(加成-消除)机制,其中从四面体中间体消除芳氧基已成为速率决定步骤。这一结果提供了在引发过程中磷酸半抗原中酚盐离子特征识别占主导地位的证据,并结合文献数据进行了讨论,这些文献数据表明一种B(Ac)2机制,对于由膦酰胺半抗原引发的抗体催化氨基甲酸酯底物水解反应,其速率决定步骤是四面体中间体的形成,其中酚盐阴离子特征最小化。本文有助于人们越来越认识到半抗原结构上的微小差异会导致催化特性上的巨大差异。